EP0957087A3 - Enzyme inhibitors - Google Patents

Enzyme inhibitors Download PDF

Info

Publication number
EP0957087A3
EP0957087A3 EP99116304A EP99116304A EP0957087A3 EP 0957087 A3 EP0957087 A3 EP 0957087A3 EP 99116304 A EP99116304 A EP 99116304A EP 99116304 A EP99116304 A EP 99116304A EP 0957087 A3 EP0957087 A3 EP 0957087A3
Authority
EP
European Patent Office
Prior art keywords
enzyme inhibitors
protecting group
amidino
intermediates
chem
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP99116304A
Other languages
German (de)
French (fr)
Other versions
EP0957087B1 (en
EP0957087A2 (en
Inventor
Karl Witold Franzmann
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Wellcome Foundation Ltd
Original Assignee
Wellcome Foundation Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GBGB9509774.7A external-priority patent/GB9509774D0/en
Application filed by Wellcome Foundation Ltd filed Critical Wellcome Foundation Ltd
Priority to EP99116304A priority Critical patent/EP0957087B1/en
Priority to SI9530645T priority patent/SI0957087T1/en
Priority to AT99116304T priority patent/ATE229001T1/en
Publication of EP0957087A2 publication Critical patent/EP0957087A2/en
Publication of EP0957087A3 publication Critical patent/EP0957087A3/en
Application granted granted Critical
Publication of EP0957087B1 publication Critical patent/EP0957087B1/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C07C317/48—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Saccharide Compounds (AREA)
  • Immobilizing And Processing Of Enzymes And Microorganisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Steroid Compounds (AREA)

Abstract

The invention relates to an intermediate of formula (VI) <CHEM> or a protected derivative thereof, wherein Q is hydrogen or a carboxyl protecting group and Q' is a protecting group. Such intermediates are useful for the preparation of amidino sulphone derivatives which, in turn, have use as selective inhibitors of inducible nitric oxide synthase.
EP99116304A 1994-06-15 1995-06-14 Intermediates useful in the preparation of enzyme inhibitors Expired - Lifetime EP0957087B1 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
EP99116304A EP0957087B1 (en) 1994-06-15 1995-06-14 Intermediates useful in the preparation of enzyme inhibitors
SI9530645T SI0957087T1 (en) 1994-06-15 1995-06-14 Intermediates useful in the preparation of enzyme inhibitors
AT99116304T ATE229001T1 (en) 1994-06-15 1995-06-14 INTERMEDIATE PRODUCTS USABLE IN THE PRODUCTION OF ENZYME INHIBITORS

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
EP94304314 1994-06-15
EP94304314 1994-06-15
GB9509774 1995-05-15
GBGB9509774.7A GB9509774D0 (en) 1995-05-15 1995-05-15 Enzyme inhibitors
EP99116304A EP0957087B1 (en) 1994-06-15 1995-06-14 Intermediates useful in the preparation of enzyme inhibitors
EP95924405A EP0765308B1 (en) 1994-06-15 1995-06-14 Enzyme inhibitors

Related Parent Applications (2)

Application Number Title Priority Date Filing Date
EP95924405A Division-Into EP0765308B1 (en) 1994-06-15 1995-06-14 Enzyme inhibitors
EP95924405A Division EP0765308B1 (en) 1994-06-15 1995-06-14 Enzyme inhibitors

Publications (3)

Publication Number Publication Date
EP0957087A2 EP0957087A2 (en) 1999-11-17
EP0957087A3 true EP0957087A3 (en) 2000-12-20
EP0957087B1 EP0957087B1 (en) 2002-12-04

Family

ID=26137155

Family Applications (2)

Application Number Title Priority Date Filing Date
EP99116304A Expired - Lifetime EP0957087B1 (en) 1994-06-15 1995-06-14 Intermediates useful in the preparation of enzyme inhibitors
EP95924405A Expired - Lifetime EP0765308B1 (en) 1994-06-15 1995-06-14 Enzyme inhibitors

Family Applications After (1)

Application Number Title Priority Date Filing Date
EP95924405A Expired - Lifetime EP0765308B1 (en) 1994-06-15 1995-06-14 Enzyme inhibitors

Country Status (29)

Country Link
US (2) USRE39576E1 (en)
EP (2) EP0957087B1 (en)
JP (2) JP2989010B2 (en)
KR (1) KR100430207B1 (en)
CN (1) CN1070849C (en)
AT (2) ATE191470T1 (en)
AU (1) AU692892B2 (en)
BR (1) BR9507995A (en)
CA (1) CA2192668A1 (en)
CY (2) CY2238B1 (en)
DE (2) DE69529101T2 (en)
DK (2) DK0765308T3 (en)
ES (2) ES2189322T3 (en)
FI (1) FI965019A (en)
GR (1) GR3033746T3 (en)
HK (1) HK1003935A1 (en)
HU (1) HUT77407A (en)
IL (2) IL114142A (en)
IS (1) IS4384A (en)
MX (1) MX9606136A (en)
MY (1) MY115437A (en)
NO (1) NO308655B1 (en)
NZ (1) NZ289157A (en)
PT (2) PT957087E (en)
RU (1) RU2162841C2 (en)
SI (2) SI0957087T1 (en)
TW (1) TW442453B (en)
WO (1) WO1995034534A1 (en)
ZA (1) ZA954940B (en)

Families Citing this family (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2740339B1 (en) * 1995-10-26 1997-12-05 Oreal USE OF AT LEAST ONE NO-SYNTHASE INHIBITOR IN THE TREATMENT OF SENSITIVE SKIN
US6369272B1 (en) 1997-01-13 2002-04-09 Glaxosmithkline Nitric oxide synthase inhibitors
US6620848B2 (en) 1997-01-13 2003-09-16 Smithkline Beecham Corporation Nitric oxide synthase inhibitors
WO1998033379A1 (en) * 1997-02-04 1998-08-06 The General Hospital Corporation A novel method for treating epidermal or dermal conditions
AU8647198A (en) * 1997-08-12 1999-03-01 Chugai Seiyaku Kabushiki Kaisha Remedies for diseases associated with bone resorption
DE69920670T2 (en) * 1998-03-11 2006-02-16 G.D. Searle & Co., Chicago HALOGENATED AMINOIC DERIVATIVES AS NITROGEN OF NITROGEN MONOXIDE SYNTHASE
US6534503B1 (en) 1998-04-28 2003-03-18 Lion Bioscience Ag Melanocortin receptor-3 ligands to treat sexual dysfunction
AU3768799A (en) 1998-04-28 1999-11-16 Trega Biosciences, Inc. Isoquinoline compound melanocortin receptor ligands and methods of using same
US6284735B1 (en) * 1998-04-28 2001-09-04 Lion Bioscience Ag HP-3228 and related peptides to treat sexual dysfunction
GB9811599D0 (en) 1998-05-30 1998-07-29 Glaxo Group Ltd Nitric oxide synthase inhibitors
AU6605800A (en) * 1999-07-16 2001-02-05 Trega Biosciences, Inc. Melanocortin receptor-3 ligands to treat sexual dysfunction
NZ520813A (en) * 2000-03-24 2004-05-28 Pharmacia Corp Amidino compounds useful as nitric oxide synthase inhibitors
AR034120A1 (en) * 2000-04-13 2004-02-04 Pharmacia Corp HALOGENATED DERIVATIVE COMPOUND OF HEPTENOIC ACID 2-AMINO-4,5, PHARMACEUTICAL COMPOSITION THAT INCLUDES IT AND THE USE OF SUCH COMPOUND AND SUCH COMPOSITION IN THE MANUFACTURE OF A MEDICINAL PRODUCT TO INHIBIT OR MODULATE NITRIC ACID SYNTHESIS
GB0031179D0 (en) * 2000-12-21 2001-01-31 Glaxo Group Ltd Nitric oxide synthase inhibitors
DE10111054A1 (en) * 2001-03-06 2002-09-12 Beiersdorf Ag Cosmetic or dermatological preparations for reinforcing skin barrier function, e.g. to prevent dryness, containing agents inhibiting the onset of nitrogen monoxide synthase activity
DE10111052A1 (en) * 2001-03-06 2002-09-12 Beiersdorf Ag Cosmetic or dermatological preparations for increasing ceramide biosynthesis, e.g. to prevent dryness, containing agents inhibiting the onset of nitrogen monoxide synthase activity
DE10111049A1 (en) * 2001-03-06 2002-09-12 Beiersdorf Ag Cosmetic or dermatological preparations for combating inflammatory disorders or dryness of the skin, containing agents inhibiting the onset of nitrogen monoxide synthase activity
DE10111050A1 (en) * 2001-03-06 2002-09-12 Beiersdorf Ag Use of substances which prevent the NO-synthase of the warm-blooded organism from exerting its effect, for the preparation of cosmetic or dermatological preparations for the treatment and / or prophylaxis of undesired skin pigmentation
US7012098B2 (en) * 2001-03-23 2006-03-14 Pharmacia Corporation Inhibitors of inducible nitric oxide synthase for chemoprevention and treatment of cancers
AU2003232148A1 (en) * 2002-05-16 2003-12-02 Pharmacia Corporation A selective inos inhibitor and a pde inhibitor in combination for the treatment of respiratory diseases
GB0214147D0 (en) * 2002-06-19 2002-07-31 Glaxo Group Ltd Formulations
DK1603872T3 (en) * 2003-03-11 2011-07-18 Pharmacia Corp S- [2 - [(1-iminoethyl) amino] ethyl] -2-methyl-1-cysteine maleate hydrochloride crystalline salt
TWI328009B (en) 2003-05-21 2010-08-01 Glaxo Group Ltd Quinoline derivatives as phosphodiesterase inhibitors
GB0316290D0 (en) 2003-07-11 2003-08-13 Glaxo Group Ltd Novel compounds
AR049384A1 (en) 2004-05-24 2006-07-26 Glaxo Group Ltd PURINA DERIVATIVES
TWI307630B (en) 2004-07-01 2009-03-21 Glaxo Group Ltd Immunoglobulins
GB0418045D0 (en) 2004-08-12 2004-09-15 Glaxo Group Ltd Compounds
EP1841780B1 (en) 2005-01-10 2011-07-27 Glaxo Group Limited Androstane 17-alpha-carbonate derivatives for use in the treatment of allergic and inflammatory conditions
AR053346A1 (en) 2005-03-25 2007-05-02 Glaxo Group Ltd COMPOSITE DERIVED FROM 8H -PIRIDO (2,3-D) PIRIMIDIN -7 ONA 2,4,8- TRISUSTITUTED PHARMACEUTICAL COMPOSITION AND USE TO PREPARE A COMPOSITION FOR TREATMENT AND PROFILXIS OF A DISEASE MEDIATED BY KINASE CSBP / RK / P38
PE20061193A1 (en) 2005-03-25 2006-12-02 Glaxo Group Ltd DERIVATIVES OF 3,4-DIHYDROPYRIMIDO [4,5-d] PYRIMIDIN-2- [1H] -0NA AS KINASE INHIBITORS p38
GB0514809D0 (en) 2005-07-19 2005-08-24 Glaxo Group Ltd Compounds
PE20071068A1 (en) 2005-12-20 2007-12-13 Glaxo Group Ltd 3- (4 - {[4- (4 - {[3- (3,3-DIMETHYL-1-PIPERIDINYL) PROPYL] OXY} PHENYL) -1-PIPERIDINYL] CARBONYL} -1-NAPHTHALENYL) PROPANOIC OR PROPENOIC ACID, SALTS OF THE SAME, AS ANTAGONISTS OF THE H1 AND H3 RECEPTORS
AR060536A1 (en) 2006-04-20 2008-06-25 Glaxo Group Ltd GLUCOCORTICOID RECEPTOR AGONIST AND PHARMACEUTICAL COMPOSITIONS
GB0611587D0 (en) 2006-06-12 2006-07-19 Glaxo Group Ltd Novel compounds
WO2008015416A1 (en) 2006-08-01 2008-02-07 Glaxo Group Limited Pyrazolo[3,4-b]pyridine compounds, and their use as pde4 inhibitors
CA2669138A1 (en) * 2006-11-09 2008-12-04 University Of Maryland, Baltimore Use of 5,6-dimethylxanthenone-4-acetic acid as an antimicrobial agent
PE20081889A1 (en) 2007-03-23 2009-03-05 Smithkline Beecham Corp INDOL CARBOXAMIDES AS INHIBITORS OF IKK2
WO2010068311A1 (en) 2008-05-23 2010-06-17 Amira Pharmaceuticals, Inc. 5-lipoxygenase-activating protein inhibitor
WO2009147190A1 (en) 2008-06-05 2009-12-10 Glaxo Group Limited Novel compounds
ES2566339T3 (en) 2008-06-05 2016-04-12 Glaxo Group Limited 4-Carboxamide indazole derivatives useful as PI3-kinase inhibitors
WO2010094643A1 (en) 2009-02-17 2010-08-26 Glaxo Group Limited Quinoline derivatives and their uses for rhinitis and urticaria
EP2406255B1 (en) 2009-03-09 2015-04-29 Glaxo Group Limited 4-oxadiazol-2-yl-indazoles as inhibitors of pi3 kinases
JP2012520257A (en) 2009-03-10 2012-09-06 グラクソ グループ リミテッド Indole derivatives as IKK2 inhibitors
US20120058984A1 (en) 2009-03-17 2012-03-08 Catherine Mary Alder Pyrimidine derivatives used as itk inhibitors
WO2010107957A2 (en) 2009-03-19 2010-09-23 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF GATA BINDING PROTEIN 3 (GATA3) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
EP2408916A2 (en) 2009-03-19 2012-01-25 Merck Sharp&Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF CONNECTIVE TISSUE GROWTH FACTOR (CTGF) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
CA2755773A1 (en) 2009-03-19 2010-09-23 Merck Sharp & Dohme Corp. Rna interference mediated inhibition of btb and cnc homology 1, basic leucine zipper transcription factor 1 (bach 1) gene expression using short interfering nucleic acid (sina)
EP2408458A1 (en) 2009-03-19 2012-01-25 Merck Sharp&Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF SIGNAL TRANSDUCER AND ACTIVATOR OF TRANSCRIPTION 6 (STAT6) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
JP2012521762A (en) 2009-03-27 2012-09-20 メルク・シャープ・エンド・ドーム・コーポレイション RNA interference-mediated inhibition of nerve growth factor β chain (NGFβ) gene expression using small interfering nucleic acids (siNA)
SG174581A1 (en) 2009-03-27 2011-10-28 Merck Sharp & Dohme RNA INTERFERENCE MEDIATED INHIBITION OF THE INTERCELLULAR ADHESION MOLECULE 1 (ICAM-1)GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
EP2411019A2 (en) 2009-03-27 2012-02-01 Merck Sharp&Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF SIGNAL TRANSDUCER AND ACTIVATOR OF TRANSCRIPTION 1 (STAT1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
EP2411520A2 (en) 2009-03-27 2012-02-01 Merck Sharp&Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF THE THYMIC STROMAL LYMPHOPOIETIN (TSLP) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
WO2010111464A1 (en) 2009-03-27 2010-09-30 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF APOPTOSIS SIGNAL-REGULATING KINASE 1 (ASK1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
JP2012524754A (en) 2009-04-24 2012-10-18 グラクソ グループ リミテッド Pyrazole and triazolcarboxamides as CRAC channel inhibitors
AR076373A1 (en) 2009-04-24 2011-06-08 Glaxo Group Ltd N-PIRAZOLIL CARBOXAMIDS AS CALCIUM CHANNEL INHIBITORS
CA2759476C (en) 2009-04-30 2018-10-09 Julie Nicole Hamblin Novel compounds
CA2777108A1 (en) * 2009-10-09 2011-04-14 Zafgen Corporation Sulphone compounds and methods of making and using same
US20120245171A1 (en) 2009-12-03 2012-09-27 Glaxo Group Limited Benzpyrazole derivatives as inhibitors of pi3 kinases
JP2013512880A (en) 2009-12-03 2013-04-18 グラクソ グループ リミテッド Indazole derivatives as PI3-kinase inhibitors
EP2507226A1 (en) 2009-12-03 2012-10-10 Glaxo Group Limited Novel compounds
EP3020393B1 (en) 2009-12-16 2020-10-07 3M Innovative Properties Company Formulations and methods for controlling mdi particle size delivery
WO2011110575A1 (en) 2010-03-11 2011-09-15 Glaxo Group Limited Derivatives of 2-[2-(benzo- or pyrido-) thiazolylamino]-6-aminopyridine, useful in the treatment of respiratoric, allergic or inflammatory diseases
GB201007203D0 (en) 2010-04-29 2010-06-16 Glaxo Group Ltd Novel compounds
PL2614058T3 (en) 2010-09-08 2015-12-31 Glaxosmithkline Ip Dev Ltd POLYMORPHS AND SALTS OF N-[5-[4-(5-{[(2R,6S)-2,6-DIMETHYL-4-MORPHOLINYL]METHYL}-& xA;1,3-OXAZOL-2-YL)-1H-INDAZOL-6-YL]-2-(METHYLOXY)-3-PYRIDINYL]METHANESULFONAMIDE
ES2602972T3 (en) 2010-09-08 2017-02-23 Glaxosmithkline Intellectual Property Development Limited Indazole derivatives for use in the treatment of influenza virus infection
WO2012035055A1 (en) 2010-09-17 2012-03-22 Glaxo Group Limited Novel compounds
EP2630127A1 (en) 2010-10-21 2013-08-28 Glaxo Group Limited Pyrazole compounds acting against allergic, inflammatory and immune disorders
US9156791B2 (en) 2010-10-21 2015-10-13 Glaxo Group Limited Pyrazole compounds acting against allergic, immune and inflammatory conditions
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
EP2683716A1 (en) 2011-03-11 2014-01-15 Glaxo Group Limited Pyrido[3,4-b]pyrazine derivatives as syk inhibitors
GB201104153D0 (en) 2011-03-11 2011-04-27 Glaxo Group Ltd Novel compounds
SG11201600028YA (en) 2013-09-22 2016-02-26 Calitor Sciences Llc Substituted aminopyrimidine compounds and methods of use
CA2943979A1 (en) 2014-03-28 2015-10-01 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
PE20170185A1 (en) 2014-05-12 2017-04-01 Glaxosmithkline Intellectual Property (No 2) Ltd PHARMACEUTICAL COMPOSITIONS TO TREAT INFECTIOUS DISEASES
GB201512635D0 (en) 2015-07-17 2015-08-26 Ucl Business Plc Uses of therapeutic compounds
US9938257B2 (en) 2015-09-11 2018-04-10 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
US10683297B2 (en) 2017-11-19 2020-06-16 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
CA3083040A1 (en) 2018-01-20 2019-07-25 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine compounds and methods of use
CA3173172A1 (en) 2020-03-26 2021-09-30 Christopher D. Kane Cathepsin inhibitors for preventing or treating viral infections

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3514450A1 (en) 1985-04-22 1986-10-23 Hoechst Ag, 6230 Frankfurt METHOD FOR PRODUCING IMIDATES AND NEW ARYL-SUBSTITUTED IMIDATES
GB9127376D0 (en) * 1991-12-24 1992-02-19 Wellcome Found Amidino derivatives
DE4310202A1 (en) * 1992-03-30 1993-10-07 Ciba Geigy Beta-keto:imido ester compsn. - used for stabilising chlorine-contg. polymer esp. PVC against heat and light
FR2727111B1 (en) * 1994-11-21 1997-01-17 Hoechst Lab NOVEL SULFUR ANALOGS OF AMINO ACIDS, THEIR PREPARATION PROCESS AND THEIR APPLICATIONS AS MEDICAMENTS

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
D. T. ELMORE ET AL.: "Kinetics and mechanism of catalysis by proteolytic enzymes", BIOCHEM. J., vol. 102, 1967, pages 728 - 734, XP000926017 *
VON P. HERMANN ET AL.: "Synthese einiger schwefelhaltiger Aminosäure-Analoga", JOURNAL FUER PRAKTISCHE CHEMIE, vol. 311, no. 6, 1969, LEIPZIG, DE, pages 1018 - 1028, XP000926022, ISSN: 0021-8383 *
VON PETER HERMANN ET AL.: "Ionisationskonstanten und Stabilitätskonstanten der Kupfer(II)-Komplexe einiger Aminosäuren und ihrer schwefelhaltigen Analoga", HOPPE-SEYLER'S Z. PHYSIOL. CHEM., vol. 349, April 1968 (1968-04-01), pages 390 - 394, XP000926019 *

Also Published As

Publication number Publication date
NZ289157A (en) 1998-03-25
JP2000026402A (en) 2000-01-25
MY115437A (en) 2003-06-30
JP3614711B2 (en) 2005-01-26
CY2455B1 (en) 2005-06-03
SI0957087T1 (en) 2003-04-30
DE69529101T2 (en) 2003-11-13
TW442453B (en) 2001-06-23
AU2891795A (en) 1996-01-05
IL114142A0 (en) 1995-10-31
EP0765308B1 (en) 2000-04-05
CN1070849C (en) 2001-09-12
USRE39576E1 (en) 2007-04-17
RU2162841C2 (en) 2001-02-10
AU692892B2 (en) 1998-06-18
KR100430207B1 (en) 2004-07-19
DK0765308T3 (en) 2000-09-11
SI0765308T1 (en) 2000-08-31
CA2192668A1 (en) 1995-12-21
HUT77407A (en) 1998-04-28
MX9606136A (en) 1998-06-30
NO965379L (en) 1996-12-13
EP0957087B1 (en) 2002-12-04
ZA954940B (en) 1996-12-17
DK0957087T3 (en) 2003-03-24
CN1155276A (en) 1997-07-23
US5889056A (en) 1999-03-30
DE69516141D1 (en) 2000-05-11
HK1003935A1 (en) 1998-11-13
ATE229001T1 (en) 2002-12-15
FI965019A0 (en) 1996-12-13
FI965019A (en) 1996-12-13
NO308655B1 (en) 2000-10-09
HU9603454D0 (en) 1997-02-28
PT957087E (en) 2003-04-30
WO1995034534A1 (en) 1995-12-21
JPH10506371A (en) 1998-06-23
IS4384A (en) 1996-11-13
DE69529101D1 (en) 2003-01-16
IL128717A0 (en) 2000-01-31
ATE191470T1 (en) 2000-04-15
BR9507995A (en) 1997-08-05
GR3033746T3 (en) 2000-10-31
EP0957087A2 (en) 1999-11-17
EP0765308A1 (en) 1997-04-02
IL114142A (en) 2000-02-17
ES2189322T3 (en) 2003-07-01
NO965379D0 (en) 1996-12-13
DE69516141T2 (en) 2000-10-19
ES2145282T3 (en) 2000-07-01
JP2989010B2 (en) 1999-12-13
PT765308E (en) 2000-09-29
CY2238B1 (en) 2003-07-04

Similar Documents

Publication Publication Date Title
EP0957087A3 (en) Enzyme inhibitors
DE69416848D1 (en) Amidino-derivate als no-synthetase inhibitoren
AU3367995A (en) New multimerizing agents
AU6645998A (en) Oxygen or sulfur containing heteroaromatics as factor xa inhibitors
IL135536A0 (en) Ortho-anthranilamide derivatives and pharmaceutical compositions containing the same
WO2003006425A3 (en) Novel compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents
AU2420897A (en) Meta-substituted phenylene sulphonamide derivatives
AU7092296A (en) Pharmaceutical compositions containing hydroximic acid derivatives
CA2203237A1 (en) Aminotetrazole derivatives useful as nitric oxide synthase inhibitors
MY128323A (en) Thiazole derivatives for inhibition of cytokine production and of cell adhesion
CA2214601A1 (en) Mercapto and seleno derivatives as inhibitors of nitric oxide synthase
EP0711164A1 (en) 4-aza-pregnane 5-alpha-reductase isozyme 1 inhibitors
IL111791A0 (en) Glutaramide derivatives
AP9400608A0 (en) &#34;New nicotinic acid derivative&#34;.
IE890257L (en) Hydrazides and hydroxamic acid derivatives
IE821943L (en) Decarboxylase-inhibiting fluorinated alkane diamine¹derivatives
CA2177586A1 (en) 4-benzoylisoxazoles and their use as herbicides
MX9604347A (en) Organic compounds.

Legal Events

Date Code Title Description
PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

Free format text: ORIGINAL CODE: 0009012

17P Request for examination filed

Effective date: 19990819

AC Divisional application: reference to earlier application

Ref document number: 765308

Country of ref document: EP

AK Designated contracting states

Kind code of ref document: A2

Designated state(s): AT BE CH DE DK ES FR GB GR IE IT LI LU MC NL PT SE

AX Request for extension of the european patent

Free format text: LT PAYMENT 19990819;LV PAYMENT 19990819;SI PAYMENT 19990819

PUAL Search report despatched

Free format text: ORIGINAL CODE: 0009013

AK Designated contracting states

Kind code of ref document: A3

Designated state(s): AT BE CH DE DK ES FR GB GR IE IT LI LU MC NL PT SE

AX Request for extension of the european patent

Free format text: LT PAYMENT 19990819;LV PAYMENT 19990819;SI PAYMENT 19990819

AKX Designation fees paid

Free format text: AT BE CH DE DK ES FR GB GR IE IT LI LU MC NL PT SE

AXX Extension fees paid

Free format text: LT PAYMENT 19990819;LV PAYMENT 19990819;SI PAYMENT 19990819

RTI1 Title (correction)

Free format text: INTERMEDIATES USEFUL IN THE PREPARATION OF ENZYME INHIBITORS

GRAG Despatch of communication of intention to grant

Free format text: ORIGINAL CODE: EPIDOS AGRA

17Q First examination report despatched

Effective date: 20020312

GRAG Despatch of communication of intention to grant

Free format text: ORIGINAL CODE: EPIDOS AGRA

GRAH Despatch of communication of intention to grant a patent

Free format text: ORIGINAL CODE: EPIDOS IGRA

GRAH Despatch of communication of intention to grant a patent

Free format text: ORIGINAL CODE: EPIDOS IGRA

GRAA (expected) grant

Free format text: ORIGINAL CODE: 0009210

AC Divisional application: reference to earlier application

Ref document number: 765308

Country of ref document: EP

AK Designated contracting states

Kind code of ref document: B1

Designated state(s): AT BE CH DE DK ES FR GB GR IE IT LI LU MC NL PT SE

AX Request for extension of the european patent

Free format text: LT PAYMENT 19990819;LV PAYMENT 19990819;SI PAYMENT 19990819

REF Corresponds to:

Ref document number: 229001

Country of ref document: AT

Date of ref document: 20021215

Kind code of ref document: T

REG Reference to a national code

Ref country code: GB

Ref legal event code: FG4D

REG Reference to a national code

Ref country code: CH

Ref legal event code: EP

REG Reference to a national code

Ref country code: IE

Ref legal event code: FG4D

REF Corresponds to:

Ref document number: 69529101

Country of ref document: DE

Date of ref document: 20030116

REG Reference to a national code

Ref country code: DK

Ref legal event code: T3

REG Reference to a national code

Ref country code: SE

Ref legal event code: TRGR

REG Reference to a national code

Ref country code: CH

Ref legal event code: NV

Representative=s name: ISLER & PEDRAZZINI AG

REG Reference to a national code

Ref country code: GR

Ref legal event code: EP

Ref document number: 20030400853

Country of ref document: GR

REG Reference to a national code

Ref country code: PT

Ref legal event code: SC4A

Free format text: AVAILABILITY OF NATIONAL TRANSLATION

Effective date: 20030303

LTIE Lt: invalidation of european patent or patent extension

Effective date: 20021204

REG Reference to a national code

Ref country code: ES

Ref legal event code: FG2A

Ref document number: 2189322

Country of ref document: ES

Kind code of ref document: T3

ET Fr: translation filed
PLBE No opposition filed within time limit

Free format text: ORIGINAL CODE: 0009261

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: NO OPPOSITION FILED WITHIN TIME LIMIT

26N No opposition filed

Effective date: 20030905

REG Reference to a national code

Ref country code: SI

Ref legal event code: IF

REG Reference to a national code

Ref country code: CH

Ref legal event code: PCAR

Free format text: ISLER & PEDRAZZINI AG;POSTFACH 1772;8027 ZUERICH (CH)

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: DK

Payment date: 20080508

Year of fee payment: 14

Ref country code: CH

Payment date: 20080425

Year of fee payment: 14

Ref country code: LU

Payment date: 20080508

Year of fee payment: 14

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: AT

Payment date: 20080507

Year of fee payment: 14

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: MC

Payment date: 20080508

Year of fee payment: 14

Ref country code: PT

Payment date: 20080414

Year of fee payment: 14

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: SE

Payment date: 20080609

Year of fee payment: 14

Ref country code: NL

Payment date: 20080530

Year of fee payment: 14

Ref country code: IE

Payment date: 20080424

Year of fee payment: 14

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: GR

Payment date: 20080411

Year of fee payment: 14

REG Reference to a national code

Ref country code: PT

Ref legal event code: MM4A

Free format text: LAPSE DUE TO NON-PAYMENT OF FEES

Effective date: 20091214

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: MC

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20090630

REG Reference to a national code

Ref country code: CH

Ref legal event code: PL

REG Reference to a national code

Ref country code: DK

Ref legal event code: EBP

NLV4 Nl: lapsed or anulled due to non-payment of the annual fee

Effective date: 20100101

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: PT

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20091214

REG Reference to a national code

Ref country code: IE

Ref legal event code: MM4A

Ref country code: SI

Ref legal event code: KO00

Effective date: 20100210

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: LI

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20090630

Ref country code: IE

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20090615

Ref country code: CH

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20090630

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: AT

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20090614

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: NL

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20100101

Ref country code: DK

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20090630

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: FR

Payment date: 20100617

Year of fee payment: 16

Ref country code: ES

Payment date: 20100618

Year of fee payment: 16

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: IT

Payment date: 20100622

Year of fee payment: 16

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: GR

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20100107

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: BE

Payment date: 20100630

Year of fee payment: 16

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: GB

Payment date: 20100401

Year of fee payment: 16

Ref country code: DE

Payment date: 20100630

Year of fee payment: 16

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: LU

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20090614

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: SE

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20090615

BERE Be: lapsed

Owner name: THE *WELLCOME FOUNDATION LTD

Effective date: 20110630

GBPC Gb: european patent ceased through non-payment of renewal fee

Effective date: 20110614

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: IT

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20110614

REG Reference to a national code

Ref country code: FR

Ref legal event code: ST

Effective date: 20120229

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: BE

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20110630

REG Reference to a national code

Ref country code: DE

Ref legal event code: R119

Ref document number: 69529101

Country of ref document: DE

Effective date: 20120103

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: DE

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20120103

Ref country code: FR

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20110630

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: GB

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20110614

REG Reference to a national code

Ref country code: ES

Ref legal event code: FD2A

Effective date: 20130604

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: ES

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20110615